Identification of covalent active site inhibitors of dengue virus protease.
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ABSTRACT:
SUBMITTER: Koh-Stenta X
PROVIDER: S-EPMC4677662 | biostudies-literature | 2015
REPOSITORIES: biostudies-literature
Publications
Identification of covalent active site inhibitors of dengue virus protease.
Koh-Stenta Xiaoying X Joy Joma J Wang Si Fang SF Kwek Perlyn Zekui PZ Wee John Liang Kuan JL Wan Kah Fei KF Gayen Shovanlal S Chen Angela Shuyi AS Kang CongBao C Lee May Ann MA Poulsen Anders A Vasudevan Subhash G SG Hill Jeffrey J Nacro Kassoum K
Drug design, development and therapy 20151210
Dengue virus (DENV) protease is an attractive target for drug development; however, no compounds have reached clinical development to date. In this study, we utilized a potent West Nile virus protease inhibitor of the pyrazole ester derivative class as a chemical starting point for DENV protease drug development. Compound potency and selectivity for DENV protease were improved through structure-guided small molecule optimization, and protease-inhibitor binding interactions were validated biophys ...[more]
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